WO2004009614A3 - Analogues de la somastatine selectifs du recepteur (sstr4) - Google Patents

Analogues de la somastatine selectifs du recepteur (sstr4) Download PDF

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Publication number
WO2004009614A3
WO2004009614A3 PCT/US2003/022600 US0322600W WO2004009614A3 WO 2004009614 A3 WO2004009614 A3 WO 2004009614A3 US 0322600 W US0322600 W US 0322600W WO 2004009614 A3 WO2004009614 A3 WO 2004009614A3
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WO
WIPO (PCT)
Prior art keywords
srif
sstr4
des
receptor
selective
Prior art date
Application number
PCT/US2003/022600
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English (en)
Other versions
WO2004009614A2 (fr
Inventor
Jean E F Rivier
Jean Claude Reubi
Judit Erchegyi
Roland Riek
Original Assignee
Salk Inst For Biological Studi
Jean E F Rivier
Jean Claude Reubi
Judit Erchegyi
Roland Riek
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Salk Inst For Biological Studi, Jean E F Rivier, Jean Claude Reubi, Judit Erchegyi, Roland Riek filed Critical Salk Inst For Biological Studi
Priority to AU2003259172A priority Critical patent/AU2003259172A1/en
Publication of WO2004009614A2 publication Critical patent/WO2004009614A2/fr
Priority to US11/041,676 priority patent/US7238775B2/en
Publication of WO2004009614A3 publication Critical patent/WO2004009614A3/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/655—Somatostatins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biophysics (AREA)
  • Medicinal Chemistry (AREA)
  • Zoology (AREA)
  • Biochemistry (AREA)
  • Toxicology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Endocrinology (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

L'invention concerne des analogues du SRIF qui sont sélectifs pour le récepteur SSTR4 contrairement aux autres récepteurs du SRIF clonés, utiles pour déterminer l'expression tissulaire et cellulaire du récepteur SSTR4 et son rôle biologique dans la régulation de la croissance tumorale. Des peptides analogues du SRIF, de type des-AA1,2,4,5,12,13 [Ala7] -SRIF; des--AA1,2,4,5,12,13 [Aph7] -SRIF, des-AA1'2,4,5,12,13 [Aph7] Cbm-SRIF; des-AA1,4,5,12,13 [Tyr2 Ala7] -Cbm-SRIF, et des-AA1'2,4,5,12,13 [Tyr7, CBMe-L-2Nal8]-SRIF, et des homologues incorporant D-Cys3 et/ou D-Trp8 et/ou Ala11, se lient avec une affinité élevée au récepteur SSTR4 humain cloné et activent celui-ci, mais ne se lient pas avec une affinité significative aux récepteurs SSTR1, SSTR2, SSTR3 ou SSTR5 humains. Par incorporation d'une tyrosine iodée en position-2 dans lesdits analogues du SRIF qui sont sélectifs pour le récepteur SSTR4, un composé marqué utile pour des méthodes de criblage de médicaments est obtenu. En variante, des cytotoxines ou des éléments hautement radioactifs peuvent être raccordés au terminal-N ou former un complexe avec celui-ci, à des fins thérapeutiques.
PCT/US2003/022600 2002-07-24 2003-07-18 Analogues de la somastatine selectifs du recepteur (sstr4) WO2004009614A2 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2003259172A AU2003259172A1 (en) 2002-07-24 2003-07-18 Receptor (sstr4)- selective somatostatin analogs
US11/041,676 US7238775B2 (en) 2002-07-24 2005-01-24 Receptor(SSTR4)-selective somatostatin analogs

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39852102P 2002-07-24 2002-07-24
US60/398,521 2002-07-24

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US11/041,676 Continuation US7238775B2 (en) 2002-07-24 2005-01-24 Receptor(SSTR4)-selective somatostatin analogs

Publications (2)

Publication Number Publication Date
WO2004009614A2 WO2004009614A2 (fr) 2004-01-29
WO2004009614A3 true WO2004009614A3 (fr) 2006-08-03

Family

ID=30771220

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/022600 WO2004009614A2 (fr) 2002-07-24 2003-07-18 Analogues de la somastatine selectifs du recepteur (sstr4)

Country Status (3)

Country Link
US (1) US7238775B2 (fr)
AU (1) AU2003259172A1 (fr)
WO (1) WO2004009614A2 (fr)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8691761B2 (en) * 2006-10-16 2014-04-08 Jean E. F. Rivier Somatostatin receptor 2 antagonists
PT2076535E (pt) 2006-10-16 2013-06-12 Univ Bern Antagonistas da somatostatina seletivos do receptor (sstr2)
WO2008095063A1 (fr) 2007-01-31 2008-08-07 Dana-Farber Cancer Institute, Inc. Peptides p53 stabilisés et utilisations de ceux-ci
KR101623985B1 (ko) 2007-03-28 2016-05-25 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 스티칭된 폴리펩티드
WO2010065572A1 (fr) 2008-12-04 2010-06-10 The Salk Institute For Biological Studies Analogues sélectifs pour sstr1
RU2582678C2 (ru) 2010-08-13 2016-04-27 Эйлерон Терапьютикс, Инк. Пептидомиметические макроциклы
TWI643868B (zh) 2011-10-18 2018-12-11 艾利倫治療公司 擬肽巨環化合物
WO2013123266A1 (fr) 2012-02-15 2013-08-22 Aileron Therapeutics, Inc. Macrocycles peptidomimétiques
CA2864120A1 (fr) 2012-02-15 2013-08-22 Aileron Therapeutics, Inc. Macrocycles peptidomimetiques reticules par triazole et par thioether
SG11201503052RA (en) 2012-11-01 2015-05-28 Aileron Therapeutics Inc Disubstituted amino acids and methods of preparation and use thereof
US10471120B2 (en) 2014-09-24 2019-11-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
CN107614003A (zh) 2015-03-20 2018-01-19 艾瑞朗医疗公司 拟肽大环化合物及其用途
WO2023250272A2 (fr) * 2022-06-24 2023-12-28 H. Lee Moffitt Cancer Center And Research Institute Inc. Molécules d'activation de lymphocytes t bispécifiques se liant à sstr

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5590656A (en) * 1992-09-15 1997-01-07 The Ohio State University Research Foundation Application of peptide/cell receptor kinetics utilizing radiolabeled somatostatin congeners in the in situ, in vivo detection and differentiation of neoplastic tissue
WO1997011962A1 (fr) * 1995-09-29 1997-04-03 Biomeasure, Incorporated Analogues peptides cycliques de somatostatine
US20020137676A1 (en) * 1998-09-01 2002-09-26 York Hsiang Selective treatment of endothelial somatostatin receptors

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US5073541A (en) 1987-11-18 1991-12-17 Administrators Of The Tulane Educational Fund Treatment of small cell lung cancer with somatostatin analogs
US5331573A (en) 1990-12-14 1994-07-19 Balaji Vitukudi N Method of design of compounds that mimic conformational features of selected peptides
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Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5590656A (en) * 1992-09-15 1997-01-07 The Ohio State University Research Foundation Application of peptide/cell receptor kinetics utilizing radiolabeled somatostatin congeners in the in situ, in vivo detection and differentiation of neoplastic tissue
WO1997011962A1 (fr) * 1995-09-29 1997-04-03 Biomeasure, Incorporated Analogues peptides cycliques de somatostatine
US20020137676A1 (en) * 1998-09-01 2002-09-26 York Hsiang Selective treatment of endothelial somatostatin receptors

Also Published As

Publication number Publication date
AU2003259172A8 (en) 2004-02-09
US20050245438A1 (en) 2005-11-03
US7238775B2 (en) 2007-07-03
AU2003259172A1 (en) 2004-02-09
WO2004009614A2 (fr) 2004-01-29

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